Influence of proline and β-Cyclodextrin in ketoconazole physicochemical and microbiological performance

Abstract

This investigation presents the characterization and evaluation of the physicochemical and microbiological properties of a new multicomponent complex of ketoconazole. Complex formation of the drug, with proline and β-cyclodextrin, was evaluated using nuclear magnetic resonance and phase solubility studies. The complex, in solid state, was prepared through kneading and physical mixture and then characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry and scanning electron microscopy. By means of confocal laser scanning microscopy, the effect of proline on the morphology of Candida albicans was evaluated. Microbiological assays were performed to evaluate the antifungal activity of the complex against C. albicans. The results obtained from phase solubility assays showed that the complexation of ketoconazole is an effective strategy to enhance its solubility. Confocal laser scanning microscopy demonstrated that proline severely affected Candida morphology, and microbiological studies established high antifungal activity for the complex, signifying an advantage, and therefore, a potential improvement in its application areas.